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Dacinostat

CAS No. : 404951-53-7

MCE 站：Dacinostat

产品活性：Dacinostat 是一种有效的 HDAC 抑制剂，IC₅₀ 值为 32 nM；Dacinostat 同时可抑制 HDAC1 的活性，IC₅₀ 值为 9 nM，主要用于癌症研究。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics  |  Autophagy

作用靶点：HDAC  |  Autophagy

In Vitro: Dacinostat (NVP-LAQ824) activates p21 promoter, with AC₅₀ of 0.30 μM. NVP-LAQ824 inhibits tumor cell (H1299, HCT116) growth, with IC₅₀s of 150 and 10 nM, respectively. NVP-LAQ824 also shows inhibitory activities against two prostate cancer cell lines (DU145 and PC3) and a breast cancer line (MDA435), with IC₅₀s of 18, 23, 39 nM, respectively. Continuous exposure of NVP-LAQ824 for 72 h produces LD90s of 0.09 M in HCT116 cells and 0.47 M in A549 cells. NVP-LAQ824 treatment of NDHF cells causes the expected G1-S growth arrest in addition to a significant reduction of cells in S-phase and accumulation of cells at the G2-M checkpoint. NVP-LAQ824 induces apoptotic death in human tumor cells. NPV-LAQ824 increases acetylation of histones H3 and H4. Dacinostat inhibits HDAC1 with an IC₅₀ of 9 nM. Dacinostat (10 and 20 nM) suppresses proliferation of AML fusion protein-expressing 32D cells. Dacinostat impairs short-term engraftment potential of leukemic stem cells. Dacinostat exhausts in vitro self-renewal potential of murine AML1/ETO- and PLZF/RARα-positive HSC.

In Vivo: NVP-LAQ824 produces a dose-dependent inhibition of tumor growth, and at 100 mg/kg, its antitumor effect is similar to that of 5-Fluorouracil.

相关产品：Covalent Screening Library Plus  |  Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Epigenetics Compound Library  |  Histone Modification Research Compound Library  |  Anti-Cancer Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Covalent Screening Library  |  Reprogramming Compound Library  |  Oxygen Sensing Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Trichostatin A  |  4-Phenylbutyric acid  |  Valproic acid  |  Entinostat  |  Sulforaphane  |  Romidepsin  |  RGFP966  |  Tasquinimod  |  Corin  |  Tacedinaline  |  ITSA-1  |  SIS17  |  Tubastatin A Hydrochloride  |  WT-161  |  Givinostat hydrochloride monohydrate  |  Pyroxamide  |  BRD-6929  |  Bufexamac  |  HDAC8-IN-1  |  Scriptaid  |  Sinapinic acid  |  Apicidin  |  BML-210  |  M344  |  Droxinostat  |  HDACs/mTOR Inhibitor 1  |  CG347B  |  Splitomicin

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